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Items: 27

1.

Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β 2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.

Koziczak-Holbro M, Rigel DF, Dumotier B, Sykes DA, Tsao J, Nguyen NH, Bösch J, Jourdain M, Flotte L, Adachi Y, Kiffe M, Azria M, Fairhurst RA, Charlton SJ, Richardson BP, Lach-Trifilieff E, Glass DJ, Ullrich T, Hatakeyama S.

J Pharmacol Exp Ther. 2019 May;369(2):188-199. doi: 10.1124/jpet.118.255307. Epub 2019 Feb 28.

PMID:
30819762
2.

2-Formylpyridyl Ureas as Highly Selective Reversible-Covalent Inhibitors of Fibroblast Growth Factor Receptor 4.

Knoepfel T, Furet P, Mah R, Buschmann N, Leblanc C, Ripoche S, Graus-Porta D, Wartmann M, Galuba I, Fairhurst RA.

ACS Med Chem Lett. 2018 Feb 1;9(3):215-220. doi: 10.1021/acsmedchemlett.7b00485. eCollection 2018 Mar 8.

3.

Bile Acid Sequestration by Cholestyramine Mitigates FGFR4 Inhibition-Induced ALT Elevation.

Schadt HS, Wolf A, Mahl JA, Wuersch K, Couttet P, Schwald M, Fischer A, Lienard M, Emotte C, Teng CH, Skuba E, Richardson TA, Manenti L, Weiss A, Graus Porta D, Fairhurst RA, Kullak-Ublick GA, Chibout SD, Pognan F, Kluwe W, Kinyamu-Akunda J.

Toxicol Sci. 2018 May 1;163(1):265-278. doi: 10.1093/toxsci/kfy031.

PMID:
29432567
4.

Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.

Fairhurst RA, Knoepfel T, Leblanc C, Buschmann N, Gaul C, Blank J, Galuba I, Trappe J, Zou C, Voshol J, Genick C, Brunet-Lefeuvre P, Bitsch F, Graus-Porta D, Furet P.

Medchemcomm. 2017 Jun 8;8(8):1604-1613. doi: 10.1039/c7md00213k. eCollection 2017 Aug 1.

5.

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Caravatti G, Guagnano V, Aichholz R, Blanz J, Blasco F, Wipfli P, Fritsch C, Maira SM, Schnell C, Seiler FH.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4729-4734. doi: 10.1016/j.bmcl.2016.08.041. Epub 2016 Aug 17.

PMID:
27575470
6.

Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.

Dickson CJ, Hornak V, Velez-Vega C, McKay DJ, Reilly J, Sandham DA, Shaw D, Fairhurst RA, Charlton SJ, Sykes DA, Pearlstein RA, Duca JS.

J Med Chem. 2016 Jun 23;59(12):5780-9. doi: 10.1021/acs.jmedchem.6b00358. Epub 2016 Jun 7.

PMID:
27239696
7.

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Fairhurst RA, Marsilje TH, Stutz S, Boos A, Niklaus M, Chen B, Jiang S, Lu W, Furet P, McCarthy C, Stauffer F, Guagnano V, Vaupel A, Michellys PY, Schnell C, Jeay S.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2057-64. doi: 10.1016/j.bmcl.2016.02.075. Epub 2016 Feb 26.

PMID:
26951753
8.

Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor.

Rosethorne EM, Bradley ME, Gherbi K, Sykes DA, Sattikar A, Wright JD, Renard E, Trifilieff A, Fairhurst RA, Charlton SJ.

Mol Pharmacol. 2016 Apr;89(4):467-75. doi: 10.1124/mol.115.101253. Epub 2016 Jan 15.

PMID:
26772612
9.

Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Imbach-Weese P, Gerspacher M, Caravatti G, Furet P, Zoller T, Fritsch C, Haasen D, Trappe J, Guthy DA, Arz D, Wirth J.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3569-74. doi: 10.1016/j.bmcl.2015.06.078. Epub 2015 Jun 27.

PMID:
26206504
10.

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Fairhurst RA, Gerspacher M, Imbach-Weese P, Mah R, Caravatti G, Furet P, Fritsch C, Schnell C, Blanz J, Blasco F, Desrayaud S, Guthy DA, Knapp M, Arz D, Wirth J, Roehn-Carnemolla E, Luu VH.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3575-81. doi: 10.1016/j.bmcl.2015.06.067. Epub 2015 Jun 26.

PMID:
26199119
11.

Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.

Gerspacher M, Fairhurst RA, Mah R, Roehn-Carnemolla E, Furet P, Fritsch C, Guthy DA.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3582-4. doi: 10.1016/j.bmcl.2015.06.077. Epub 2015 Jun 30.

PMID:
26164189
12.

The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.

Arnold N, Beattie D, Bradley M, Brearley A, Brown L, Charlton SJ, Fairhurst RA, Farr D, Fozard J, Fullerton J, Gosling M, Hatto J, Janus D, Jones D, Jordan L, Lewis C, Maas J, McCarthy C, Mercer M, Oakman H, Press N, Profit R, Schuerch F, Sykes D, Taylor RJ, Trifilieff A, Tuffnell A.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4341-7. doi: 10.1016/j.bmcl.2014.06.014. Epub 2014 Jun 26.

PMID:
25065493
13.

Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor.

Sykes DA, Parry C, Reilly J, Wright P, Fairhurst RA, Charlton SJ.

Mol Pharmacol. 2014 Apr;85(4):608-17. doi: 10.1124/mol.113.090209. Epub 2014 Jan 29.

PMID:
24476583
14.

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R, Hamon J, Fabbro D, Caravatti G.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. doi: 10.1016/j.bmcl.2013.05.007. Epub 2013 May 14. Erratum in: Bioorg Med Chem Lett. 2013 Aug 15;23(16):4723.

PMID:
23726034
15.

An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.

Beattie D, Beer D, Bradley ME, Bruce I, Charlton SJ, Cuenoud BM, Fairhurst RA, Farr D, Fozard JR, Janus D, Rosethorne EM, Sandham DA, Sykes DA, Trifilieff A, Turner KL, Wissler E.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6280-5. doi: 10.1016/j.bmcl.2012.07.096. Epub 2012 Aug 4.

PMID:
22932315
16.

Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists.

Rosethorne EM, Turner RJ, Fairhurst RA, Charlton SJ.

Naunyn Schmiedebergs Arch Pharmacol. 2010 Sep;382(3):255-63. doi: 10.1007/s00210-010-0533-6. Epub 2010 Aug 8.

PMID:
20694793
17.

A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.

Beattie D, Bradley M, Brearley A, Charlton SJ, Cuenoud BM, Fairhurst RA, Gedeck P, Gosling M, Janus D, Jones D, Lewis C, McCarthy C, Oakman H, Stringer R, Taylor RJ, Tuffnell A.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5302-7. doi: 10.1016/j.bmcl.2010.06.136. Epub 2010 Jul 1.

PMID:
20655218
18.

The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.

Baur F, Beattie D, Beer D, Bentley D, Bradley M, Bruce I, Charlton SJ, Cuenoud B, Ernst R, Fairhurst RA, Faller B, Farr D, Keller T, Fozard JR, Fullerton J, Garman S, Hatto J, Hayden C, He H, Howes C, Janus D, Jiang Z, Lewis C, Loeuillet-Ritzler F, Moser H, Reilly J, Steward A, Sykes D, Tedaldi L, Trifilieff A, Tweed M, Watson S, Wissler E, Wyss D.

J Med Chem. 2010 May 13;53(9):3675-84. doi: 10.1021/jm100068m.

PMID:
20402514
19.

Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.

Beattie D, Brearley A, Brown Z, Charlton SJ, Cox B, Fairhurst RA, Fozard JR, Gedeck P, Kirkham P, Meja K, Nanson L, Neef J, Oakman H, Spooner G, Taylor RJ, Turner RJ, West R, Woodward H.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1219-24. doi: 10.1016/j.bmcl.2009.11.131. Epub 2009 Dec 1.

PMID:
20031406
20.

7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.

Sandham DA, Adcock C, Bala K, Barker L, Brown Z, Dubois G, Budd D, Cox B, Fairhurst RA, Furegati M, Leblanc C, Manini J, Profit R, Reilly J, Stringer R, Schmidt A, Turner KL, Watson SJ, Willis J, Williams G, Wilson C.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. doi: 10.1016/j.bmcl.2009.06.042. Epub 2009 Jun 14.

PMID:
19592244
21.

Potent and selective xanthine-based inhibitors of phosphodiesterase 5.

Arnold NJ, Arnold R, Beer D, Bhalay G, Collingwood SP, Craig S, Devereux N, Dodds M, Dunstan AR, Fairhurst RA, Farr D, Fullerton JD, Glen A, Gomez S, Haberthuer S, Hatto JD, Howes C, Jones D, Keller TH, Leuenberger B, Moser HE, Muller I, Naef R, Nicklin PA, Sandham DA, Turner KL, Tweed MF, Watson SJ, Zurini M.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2376-9. Epub 2006 Nov 10.

PMID:
17337182
22.

Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi.

Naline E, Trifilieff A, Fairhurst RA, Advenier C, Molimard M.

Eur Respir J. 2007 Mar;29(3):575-81. Epub 2006 Nov 29.

23.

In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action.

Battram C, Charlton SJ, Cuenoud B, Dowling MR, Fairhurst RA, Farr D, Fozard JR, Leighton-Davies JR, Lewis CA, McEvoy L, Turner RJ, Trifilieff A.

J Pharmacol Exp Ther. 2006 May;317(2):762-70. Epub 2006 Jan 24.

PMID:
16434564
24.

Synthesis of the marine sponge derived beta2-adrenoceptor agonist S1319.

Fairhurst RA, Janus D, Lawrence A.

Org Lett. 2005 Oct 13;7(21):4697-700.

PMID:
16209513
25.

Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.

Alikhani V, Beer D, Bentley D, Bruce I, Cuenoud BM, Fairhurst RA, Gedeck P, Haberthuer S, Hayden C, Janus D, Jordan L, Lewis C, Smithies K, Wissler E.

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4705-10.

PMID:
15324892
26.

Two [7.3.1]azabicyclo-z-3-ene-1,5-diyne analogues of dynemicin A.

Lynch VM, Fairhurst RA, Iliadis TN, Magnus P, Davis BE.

Acta Crystallogr C. 1995 Apr 15;51 ( Pt 4):782-6.

PMID:
7619344
27.

4,7-Dimethoxybenzo[c]furan.

Lynch VM, Fairhurst RA, Magnus P, Davis BE.

Acta Crystallogr C. 1995 Apr 15;51 ( Pt 4):780-2.

PMID:
7619343

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